摘要:
An enzymatically active reusable sponge or foam, capable of regeneration with oximes, made of a polymer such as polyurethane is prepared for detoxification of hazardous compounds such as organophosphorus and organosulfur compounds. The foam or sponge contains a plurality of enzymes including enzymes selected from acetylcholinesterase, butyrylcholinesterase, triesterase, pseudocholinesterase, organophosphate hydrase, phosphotriesterase, paraoxonase and organophosphorus and organosulfur hydrolyzing enzymes. The sponge or foam may additionally contain activated carbon and an enzyme reactivation compound. A kit can be formed containing the sponge or foam and the compound for enzyme reactivation. The enzymatically active foam or sponge may be prepared using a two chamber device where enzymes and prepolymer are passed from separate chambers into a static mixing stator and are subjected to low shear mixing and extrusion to form by the sponge or foam.
摘要:
Methods, compositions and materials useful in the detection of organophosphorous and organosulfur compounds are disclosed. In particular, biosensors wherein a porous or a non-porous support having an enzyme immobilized upon or within are disclosed. The biosensors exhibit enzymatic stability at extreme temperatures and/or denaturing conditions, and similar kinetic characteristics of the soluble form of the enzymes utilized. The enzyme does not leach from the porous or non-porous support and the material retains enzymatic activity after prolonged storage. Differential biosensors are also disclosed.
摘要:
An assay for detecting, measuring, or monitoring the activity or concentration of at least two proteins that have similar or overlapping properties is disclosed. The assay comprises first determining the sensitivity coefficients of the substrates for each of the proteins in which the concentrations are to be determined. This method may be used for detecting, measuring, or monitoring the activity and concentration of AChE, BChE, or both in a test sample which test sample may be whole and unprocessed blood or tissue. Also disclosed are methods of using the assay to detect a subject's exposure to an agent which affects cholinesterase, determine the efficacy or progress of a treatment, determine the amount of protection provided against exposure to an agent which affects cholinesterase, or both, screen a subject for having a drug sensitivity or a particular disease, detect a change in red blood cell count of a subject, determine whether a candidate compound affects cholinesterase. Also disclosed are devices and kits for detecting, measuring, or monitoring the activities and concentrations of AChE, BChE, or both.
摘要:
A novel targeting peptide from the C-terminal of endothelin and/or a novel fusogenic peptide from hemagglutinin are optionally conjugated to the carboxy group of 1,2-dioleoyl-sn-glycero-3-succinate and incorporated into liposomes for therapeutic treatment. The novel targeting peptide directs liposomes to lung cells, and, therefore, is useful for delivering liposomes encapsulating cholinesterase genes, particularly, the human serum butyryl cholinesterase (Hu BChE) gene, as a treatment against nerve agents. It is emphasized that this abstract is provided to comply with the rules requiring an abstract which will allow a searcher or other reader quickly to ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope or meaning of the appended issued claims. 37 CFR §1.72(b).
摘要:
A receptor ligand is conjugated to a lipid-soluble moiety, thereby allowing effective delivery of the peptide ligand to a target cell in the form of a liposome complex. The ligand brings the liposome in proximity to the target cell, facilitating the fusion of the liposome with an endosome of the cellular target to release the payload into the cytoplasm. The liposome itself packages drugs or other therapeutics that are delivered to the interior of the cell upon fusion of the liposome.
摘要:
Disclosed herein are methods for the large-scale preparation of human butyrylcholinesterase (HuBChE) preparations from Cohn Fraction IV-4. As disclosed, the methods provide HuBChE preparations that are about 99% or more pure with recovery yields of about 60%. Also disclosed are the pharmacokinetics, safety and toxicity, stability and efficacy of the HuBChE preparations.
摘要:
The compounds of the invention are generally described by the formula (1): B1Z*2B3Z*4X*5Q6F7X8X9X10X11, (2): B1X2X3X4X5Q6F7X8X9X10X11, or (3): B1X2B3X4Z5Q6F7Z8X9X10X11 and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic or polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large or hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum B and tetanus toxins.
摘要翻译:本发明的化合物通常由式(1)描述:B 1 Z * 2 B 3 Z * 4 < 5×6×6×6××××××××××××××××××××××××××××××××××××××××××< (2):B 1 X 2 X 3 X 2 X 2 X 3 5 i> 5 i> 5 i> i> i> 或(3):B 1 X 2 B 3 3 5 u> X u> 5 u> 5 i> 5 i> 它们的盐,酯,酰胺和酰基形式。 由字母表示的每个位置表示单个氨基酸残基:B是碱性或极性/大氨基酸或其修饰形式; X是小或疏水性氨基酸或其修饰形式; X *是小或极/大氨基酸或其修饰形式; Z是极性/大或疏水性氨基酸或其修饰形式; Z *是脯氨酸或极性/大或疏水性氨基酸或其修饰形式。 如下所述,氨基酸残基之间的一个或多个肽键可以被肽键模拟物代替。 这些化合物可用作分子结构单元以产生针对抑制肉毒杆菌B和破伤风毒素的蛋白酶活性而优化的化合物。
摘要:
The compounds of the invention are generally described by the formula: B1Z*2B3Z*4X*5Q6F7X8X9X10X11, (1) B1X2X3X4X5Q6F7X8X9X10X11, or (2) B1Z2B3X4Z5Q6F7Z8X9X10X11 (3) and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic of polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large of hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum b and tetanus toxins.
摘要:
The compounds of the invention are generally described by the formula: B1Z*2B3Z*4X*5Q6F7X8X9X10X11 (1), B1X2X3X4X5Q6F7X8X9X10X11 (2), or B1X2B3X4Z5Q6F7Z*8X9X10X11 (3) and the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic or polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large or hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum B and tetanus toxins.
摘要翻译:本发明的化合物通常用下式描述:或其盐,酯,酰胺及其酰基形式。 由字母表示的每个位置表示单个氨基酸残基:B是碱性或极性/大氨基酸或其修饰形式; X是小或疏水性氨基酸或其修饰形式; X *是小或极/大氨基酸或其修饰形式; Z是极性/大或疏水性氨基酸或其修饰形式; Z *是脯氨酸或极性/大或疏水性氨基酸或其修饰形式。 如下所述,氨基酸残基之间的一个或多个肽键可以被肽键模拟物代替。这些化合物可以用作分子结构单元以产生针对抑制肉毒杆菌B和破伤风的蛋白酶活性而优化的化合物 毒素
摘要:
The compounds of the invention are generally described by the formula: X1X2B3X4B5X*6X7X8 B9X10B11X12B13X14 B15X16B17X*18X*19B20 X21X22X23Q24F25Z*26X27 X28B29X30B31B32X33X34 B35B36X37Z38Z39 (1) and the salts, esters, amides, and acyl forms thereof. Up to 15 amino acids may be truncated from the N-terminus and up to 6 amino acids may be truncated from the C-terminus. Each position represented by a letter indicates a single amino acid residue wherein B is a basic or polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large or hydrophobic amino acid or a modified form thereof. These compounds may be used to inhibit the protease activity of Botulinum B and tetanus toxins.
摘要翻译:本发明的化合物通常用下式描述:及其盐,酯,酰胺及其酰基形式。 可以从N末端截断至多15个氨基酸,并且可以从C末端截断至多6个氨基酸。 由字母表示的每个位置表示单个氨基酸残基,其中B是碱性或极性/大氨基酸或其修饰形式; X是小或疏水性氨基酸或其修饰形式; X *是小或极/大氨基酸或其修饰形式; Z是极性/大或疏水性氨基酸或其修饰形式; Z *是脯氨酸或极性/大或疏水性氨基酸或其修饰形式。 这些化合物可用于抑制肉毒杆菌B和破伤风毒素的蛋白酶活性。